ABSTRACT
OBJECTIVE: To prepare ropivacaine ethosomal gel and study its transdermal permeation. METHODS: The ropivacaine ethosomes were prepared by ethanol injection method. The formulation and the preparation method of ethosomes were optimized by orthogonal experiment. The particle size, morphology and encapsulation efficiency were evaluated, and the carbomer was added as the base for the preparation of the ethosomal gel. The penetration experiments of ropivacaine ethosomal gel through mouse skin were performed by Franz's cell. The cumulative penetration amount was calculated. RESULTS: The obtained ethosomes were approximately spherical, the size were (127.6±4.8) nm. The entrapment efficiency of ropivacaine in ethosomes was (77.58±1.07)%. Accumulative permeation amount of ropivacaine ethosomal gel within 24 h was 73.07 μg·cm-2, which was about 1.56 times of normal gel. CONCLUSION: The gel is feasible in preparation technique, controllable in quality and can significantly promote transdermal penetration of ropivacaine.
ABSTRACT
OBJECTIVE: To prepare lornoxicam (LN) ethosomal gel and to study its transdermal permeation in vitro. METHODS: The LN ethosomes were prepared by ethanol injection method. The formulation and the preparation method of ethosomes were optimized by orthogonal experiment using encapsulation efficiency as index. The morphology, particle size, Zeta potential and entrapment efficiency were evaluated, and the carbomer was added as the base for the preparation of the ethosomal gel. The penetration experiments of LN ethosomal gel through mouse skin were performed by Franz's cell. The concentration of LN was determined by HPLC. The cumulative penetration amount, steady penetration rate and the skin deposition of the drug were calculated. RESULTS: The obtained ethosomes were spherical, the mean size and Zeta potential were (385.6 ± 59.2) nm and (-23.49 ± 2.38) mV, respective-ly. The mean entrapment efficiency of LN in ethosomes was (73.44 ± 1.35)%. The LN ethosomal gel had a translucent yellow viscous colloidal appearance. The steady penetration rate of LN from ethosomal gel (2.81 μg · cm-2 · h-1) was 12.77, 3.51 and 2.60 times higher than that from suspensions, gel and hydroethanolic suspensions of LN, respectively. The skin deposition of the drug at the end of the experiment was statistically greater from the ethosomal gel than from other control groups. CONCLUSION: The gel is feasible in preparation technique, stable and controllable in quality and can improve transdermal penetration and increased the LN amount retain in the skin significantly.
ABSTRACT
OBJECTIVE: In vivo study on the oxybutynin hydrochloride (OXB) ethosomal gel in rabbits was carried out to obtain pharmacokinetic parameters in comparison to contrast gel. METHODS: After transdermal administration in rabbits of the OXB ethosomal gel and contrast gel respectively, OXB in the plasma was determined by HPLC-MS, the pharmacokinetic parameters were calculated with DAS 2.1.1. RESULTS: Dose of OXB for 20 mg in the ethosomal gel and for 50 mg in contrast gel transdermal delivery, the AUC0→48 of ethosomal gel and contrast gel were 597.63, 518.40 ng · h · mL-1, ρmax were 27.91, 29.81 ng · mL-1, and tmax were 6.67, 4.67 h respectively. A relative bioavailability of OXB ethosomal gel was 288.4% compared with contrast gel. CONCLUSION: In vivo experiments indicate that the OXB ethosomal gel not only reduce the drug dosage, but also show good bioavailability in rabbits.